Id: acc0201
Group: 2sens
Protein: JAK2
Gene Symbol: JAK2
Protein Id: O60674
Protein Name: JAK2_HUMAN
PTM: phosphorylation
Site: Tyr1007
Site Sequence: TKVLPQDKEYYKVKEPGESPI
Disease Category: Cancer
Disease: Prostate Cancer
Disease Subtype:
Disease Cellline: DU145
Disease Info:
Drug: EC-70124
Drug Info: "Epirubicin is an anthracycline chemotherapeutic agent that inhibits cancer cell growth by interfering with DNA replication and cell division, primarily used in the treatment of breast cancer, ovarian cancer, and gastric cancer. Cyclophosphamide is an alkylating agent that suppresses DNA and RNA synthesis, exhibiting both antineoplastic and immunomodulatory effects, often combined with epirubicin in EC chemotherapy regimens to enhance efficacy and reduce drug resistance. "
Effect: modulate
Effect Info: "EC - 70124 inhibits the phosphorylation of IκB, STAT3 (Tyr705) and JAK2 (Tyr1007/1008), thereby suppressing tumors."
Note:
Score: 4.0
Pubmed(PMID): 26826115
Sentence Index:
Sentence:

Sequence & Structure:

MGMACLTMTEMEGTSTSSIYQNGDISGNANSMKQIDPVLQVYLYHSLGKSEADYLTFPSGEYVAEEICIAASKACGITPVYHNMFALMSETERIWYPPNHVFHIDESTRHNVLYRIRFYFPRWYCSGSNRAYRHGISRGAEAPLLDDFVMSYLFAQWRHDFVHGWIKVPVTHETQEECLGMAVLDMMRIAKENDQTPLAIYNSISYKTFLPKCIRAKIQDYHILTRKRIRYRFRRFIQQFSQCKATARNLKLKYLINLETLQSAFYTEKFEVKEPGSGPSGEEIFATIIITGNGGIQWSRGKHKESETLTEQDLQLYCDFPNIIDVSIKQANQEGSNESRVVTIHKQDGKNLEIELSSLREALSFVSLIDGYYRLTADAHHYLCKEVAPPAVLENIQSNCHGPISMDFAISKLKKAGNQTGLYVLRCSPKDFNKYFLTFAVERENVIEYKHCLITKNENEEYNLSGTKKNFSSLKDLLNCYQMETVRSDNIIFQFTKCCPPKPKDKSNLLVFRTNGVSDVPTSPTLQRPTHMNQMVFHKIRNEDLIFNESLGQGTFTKIFKGVRREVGDYGQLHETEVLLKVLDKAHRNYSESFFEAASMMSKLSHKHLVLNYGVCVCGDENILVQEFVKFGSLDTYLKKNKNCINILWKLEVAKQLAWAMHFLEENTLIHGNVCAKNILLIREEDRKTGNPPFIKLSDPGISITVLPKDILQERIPWVPPECIENPKNLNLATDKWSFGTTLWEICSGGDKPLSALDSQRKLQFYEDRHQLPAPKWAELANLINNCMDYEPDFRPSFRAIIRDLNSLFTPDYELLTENDMLPNMRIGALGFSGAFEDRDPTQFEERHLKFLQQLGKGNFGSVEMCRYDPLQDNTGEVVAVKKLQHSTEEHLRDFEREIEILKSLQHDNIVKYKGVCYSAGRRNLKLIMEYLPYGSLRDYLQKHKERIDHIKLLQYTSQICKGMEYLGTKRYIHRDLATRNILVENENRVKIGDFGLTKVLPQDKEYYKVKEPGESPIFWYAPESLTESKFSVASDVWSFGVVLYELFTYIEKSKSPPAEFMRMIGNDKQGQMIVFHLIELLKNNGRLPRPDGCPDEIYMIMTECWNNNVNQRPSFRDLALRVDQIRDNMAG

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
JAK2 BARICITINIB Tyrosine-protein kinase JAK2 inhibitor 4 - immune system disease ATC
JAK2 FILGOTINIB Tyrosine-protein kinase JAK2 inhibitor 4 - immune system disease ATC
JAK2 RUXOLITINIB Tyrosine-protein kinase JAK2 inhibitor 4 - neoplasm ATC
JAK2 PACRITINIB Tyrosine-protein kinase JAK2 inhibitor 4 - neoplasm ATC
JAK2 FEDRATINIB Tyrosine-protein kinase JAK2 inhibitor 4 - neoplasm ATC
JAK2 TOFACITINIB CITRATE Janus Kinase (JAK) inhibitor 4 - rheumatoid arthritis DailyMed
DailyMed
JAK2 BARICITINIB Tyrosine-protein kinase JAK2 inhibitor 4 - rheumatoid arthritis FDA
DailyMed
EMA
JAK2 TOFACITINIB CITRATE Janus Kinase (JAK) inhibitor 4 Recruiting rheumatoid arthritis ClinicalTrials
JAK2 BARICITINIB Tyrosine-protein kinase JAK2 inhibitor 4 Recruiting rheumatoid arthritis ClinicalTrials
ClinicalTrials
ClinicalTrials
JAK2 BARICITINIB Tyrosine-protein kinase JAK2 inhibitor 4 Terminated rheumatoid arthritis ClinicalTrials
JAK2 BARICITINIB Tyrosine-protein kinase JAK2 inhibitor 4 Active, not recruiting rheumatoid arthritis ClinicalTrials
JAK2 BARICITINIB Tyrosine-protein kinase JAK2 inhibitor 4 Completed rheumatoid arthritis ClinicalTrials
JAK2 FILGOTINIB MALEATE Tyrosine-protein kinase JAK2 inhibitor 4 - rheumatoid arthritis EMA
JAK2 UPADACITINIB HEMIHYDRATE Tyrosine-protein kinase JAK2 inhibitor 4 - rheumatoid arthritis FDA
DailyMed
JAK2 PACRITINIB CITRATE Tyrosine-protein kinase JAK2 inhibitor 4 - primary myelofibrosis FDA
JAK2 RUXOLITINIB PHOSPHATE Tyrosine-protein kinase JAK2 inhibitor 4 - polycythemia vera EMA
DailyMed
JAK2 PACRITINIB CITRATE Tyrosine-protein kinase JAK2 inhibitor 4 - polycythemia vera FDA
JAK2 RUXOLITINIB PHOSPHATE Tyrosine-protein kinase JAK2 inhibitor 4 - primary myelofibrosis DailyMed
JAK2 FEDRATINIB HYDROCHLORIDE Tyrosine-protein kinase JAK2 inhibitor 4 - primary myelofibrosis FDA
EMA
JAK2 TOFACITINIB CITRATE Janus Kinase (JAK) inhibitor 4 - psoriatic arthritis DailyMed
JAK2 RUXOLITINIB PHOSPHATE Tyrosine-protein kinase JAK2 inhibitor 4 - myeloproliferative disorder EMA
JAK2 FEDRATINIB HYDROCHLORIDE Tyrosine-protein kinase JAK2 inhibitor 4 - myeloproliferative disorder EMA
JAK2 RUXOLITINIB Tyrosine-protein kinase JAK2 inhibitor 4 - Eczematoid dermatitis ATC
JAK2 FEDRATINIB HYDROCHLORIDE Tyrosine-protein kinase JAK2 inhibitor 4 - Myelofibrosis DailyMed
JAK2 RUXOLITINIB PHOSPHATE Tyrosine-protein kinase JAK2 inhibitor 4 - Myelofibrosis DailyMed

Note: Only show clinically investigational or approved drugs with protein targets.

Protein Tractability:

source: Open Targets
Small molecule
Antibody
PROTAC
Other modalities
Approved Drug
Advanced Clinical
Phase 1 Clinical
Structure with Ligand
High-Quality Ligand
High-Quality Pocket
Med-Quality Pocket
Druggable Family
Approved Drug
Advanced Clinical
Phase 1 Clinical
UniProt loc high conf
GO CC high conf
UniProt loc med conf
UniProt SigP or TMHMM
GO CC med conf
Human Protein Atlas loc
Approved Drug
Advanced Clinical
Phase 1 Clinical
Literature
UniProt Ubiquitination
Database Ubiquitination
Half-life Data
Small Molecule Binder
Approved Drug
Advanced Clinical
Phase 1 Clinical

PTM Intensity:

source: CPTAC
JAK2-Tyr570
Cancer Intensity
BRCA
COAD
HGSC
ccRCC
GBM -0.417
HNSC -0.724
LUAD
LUSC 1.141
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
Y 1007 U Prostate cancer/carcinoma/adenocarcinoma Phosphorylation 22307624

State Note: Based on the distinct PTM states in diseases, PTMD classified all disease-associated PTMs into six classes, including whether the up-regulation (U) or down-regulation (D) of PTM levels, the absence (A) or presence (P) of PTMs, and the creation (C) or disruption (N) of PTM sites are associated with diseases.

PTM-Drug Perturbation Response:

source: DecryptM

No data.

Function score:

source: funscoR

No data.

Cross Links: